Antinociceptive, anti-inflammatory, and central nervous system (CNS) effects of the natural coumarin soulattrolide

Drug Dev Res. 2018 Nov;79(7):332-338. doi: 10.1002/ddr.21471. Epub 2018 Sep 23.

Abstract

Soulattrolide is a natural coumarin synthesized by the leaves of species of Calophyllum (Calophyllaceae) rain forest trees, including the American C. brasiliense, and the Asian C. teysmanii. Soulattrolide is a potent inhibitor of the reverse transcriptase from HIV-1 (RT-HIV-1), and active against Mycobacterium tuberculosis. However, the effects of this coumarins on other systems, remains to be evaluated. C. brasiliense is used in traditional medicine for the treatment of pain and inflammation. Therefore, we decided to explore the antinociceptive, anti-inflammatory activity of soulattrolide in mice, as well as, some of its possible effects on the CNS. Soulattrolide showed antinociceptive effects in the writhing test (ED50 = 33.8 mg/kg), as well as, in the formalin test with an ED50 = 7.9, and 22.1 mg/kg for Phases 1 and 2, respectively. The highest dose of soulattrolide (50 mg/kg) induced 40% of antinociception in the hot plate test. Regarding to anti-inflammatory activity, in the 12-O-Tetradecanoylphorbol-13-acetate (TPA) test, soulattrolide showed an IC50 = 1.81 μmol/ear, whereas in the myeloperoxidase assay, it showed an inhibition of 87% (1 μmol/ear). Soulattrolide showed sedative effects on the pentobarbital-induced sleeping time test, and the rotarod test, but lacked antidepressant activity on the tail suspension test. In conclusion, we report for the first time, the antinociceptive effects of soulattrolide in mice, like those of naproxen; soulattrolide also showed mild anti-inflammatory activity, as well as mild sedative and anxiolytic properties, therefore, it has also activity on the CNS.

Keywords: Calophyllum brasiliense; antinociceptive; anxiolytic; central nervous system; soulattrolide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Animals
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology*
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Central Nervous System Agents / chemistry
  • Central Nervous System Agents / pharmacology*
  • Coumarins / chemistry
  • Coumarins / pharmacology*
  • Dose-Response Relationship, Drug
  • Hypnotics and Sedatives / chemistry
  • Hypnotics and Sedatives / pharmacology
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Pain Measurement / drug effects*
  • Pain Measurement / methods

Substances

  • Analgesics
  • Anti-Anxiety Agents
  • Anti-Inflammatory Agents
  • Central Nervous System Agents
  • Coumarins
  • Hypnotics and Sedatives
  • soulattrolide
  • coumarin